Background: To understand the cumulative effect of topical formulations after medication, evaluate the therapeutic effect of microneedle-assisted (MN-assisted) paeoniflorin-loaded ethosomes (TGP-E), and explore the potential for deep penetration of drugs, this paper uses microdialysis to systematically study the percutaneous pharmacokinetics of TGP-E.
Methods: First, optical coherence tomography (OCT) was used to study the effectiveness of microneedle puncture. Second, a microdialysis method and a UPLC-MS method for determining the amount of paeoniflorin (Pae) in dialysate were established. Finally, the transdermal pharmacokinetics of TGP-E was studied using in vivo microdialysis in rats under the above MN-assisted conditions.
Results: The optimal MN-assisted conditions were obtained at a microneedle length of 500 μm, a pressure of 3 N, and an action time of 3 min. The pharmacokinetic results demonstrated that the maximum drug concentration (Cmax) and the area under the curve (AUC) of the TGP-E gel were higher than the TGP-saline solution gel, and the mean retention time was lower. These indicated that microneedle can promote the entry of the ethosomes into the skin for in vivo experiments and greatly improve the possibility of deep penetration of the water-soluble Pae.
Conclusion: Therefore, the microneedle-ethosomes delivery system is a more ideal means for promoting the deep penetration of Pae. These findings may provide a reference for the combination of multiple penetration-enhancement ways to promote drug absorption, and also provide a new insight to realize the development of novel, safe, and more effective dosage forms and administration routes of drugs.
Background: Ablative fractional carbon dioxide laser (AFCO2) resurfacing causes transient skin barrier disruption characterized by decreased skin hydration and increased transepidermal water loss (TEWL). Snail Soothing and Repairing (SSR) cream, containing several glycoproteins with potential antimicrobial and antioxidant effects, may benefit skin hydration promotion after the laser treatment.
Objective: To evaluate the efficacy and safety of SSR cream in skin hydration promotion after AFCO2 resurfacing.
Method: The study was a double-blinded, split-face, placebo-controlled trial in participants aged 18-50 years with atrophic acne scars on both cheeks. After AFCO2 resurfacing, participants applied the product or placebo on either cheek twice daily for 14 days. Corneometry, TEWL, colorimetry, and clinical assessments (edema, erythema, crusting, pruritus, and tightness score) were evaluated at baseline, day 7, and day 14 after AFCO2 resurfacing.
Results: From 22 participants in the study, the SSR cream-treated sides showed significantly higher corneometry levels than placebo-treated sides at day 14 (p = 0.033), while TEWL and colorimetry levels were not different at any study visits. Pruritus and tightness scores of the SSR side were lower, but not significant, than the placebo. Other clinical assessments (edema, erythema, and crusting) showed similar results. No significant adverse events took place.
Conclusion: The SSR cream significantly improved skin hydration, highlighting skin barrier restoration after AFCO2 resurfacing, with a good safety profile.
Introduction: Pattern recognition receptors are involved in innate and adaptive immunity by detecting microbial components. Bacteria have been accused to play a role in inflammatory acne. We investigated the potential involvement of Toll-like receptor (TLR)2, TLR4, TLR6, and CD14 in the direct influence of bacterial components and standard antiacne compounds on human sebocytes.
Methods: mRNA and protein expression of TLR2, TLR4, TLR6, and CD14 in SZ95 sebocytes was evaluated by real-time qRT-PCR and immunocytochemistry. The effects of lipopolysaccharides (LPS) and lipoteichoic acid on TLR2, TLR4, and CD14 expression and of cytokine/chemokine secretion by 13-cis-retinoic acid, all-trans-retinoic acid, retinol, and hydrocortisone at the mRNA and protein levels were assessed by real-time qRT-PCR and ELISA and verified by cocultivation with neutralizing antibodies.
Results: The constitutive expression of TLR2, TLR4, and CD14 in SZ95 sebocytes was augmented by exposure to LPS. Hydrocortisone induced TLR2, but markedly reduced TLR4 expression. 13-cis-retinoic acid and all-trans-retinoic acid regulated IL-6 release. LPS enhanced and hydrocortisone reduced cytokine and chemokine release. Anti-TLR4 and anti-CD14 mAb blocked LPS-induced IL-8 and IL-6 release.
Conclusions: Microbial components use pattern recognition receptors to directly activate sebocytes to express a wide range of proinflammatory molecules and especially IL-8 and IL-6 in a TLR4- and CD14-specific manner. Retinoids, but mostly corticosteroids, also use this pathway to exhibit anti-inflammatory effects.
Background/objective: Hair cycle is regulated by many biological factors. Cathepsins are involved in various physiological processes in human skin. Here, we investigated the cathepsin expression and distribution changes in follicular growth cycles for better understanding the hair cycles and to explore new intervention measures.
Methods: The 24 mice (C57BL/6, female, 7-week old) were selected and removed the back hair via rosin/paraffin method. At Day 8, Day 20, and Day 25, biopsy on post-plucking area was done. Immunohistochemical staining, Western blot, and Q-PCR were used to test the cathepsin B/D/L/E.
Results: In anagen, cathepsins (B, D, L, and E) were distributed in the hair follicle matrix, inner hair root sheath, and hair. In catagen, cathepsins were mainly observed in un-apoptosis inner root sheath and outer root sheath. Expression of cathepsins B-mRNA and L-mRNA was decreased from anagen and catagen to telogen. Cathepsin D-mRNA was increased in catagen and then decreased in telogen. Cathepsin E-mRNA was decreased in catagen and slightly increased in telogen.
Conclusions: The distribution and expression of cathepsins B, D, L, and E in hair follicle changed with hair growth process which indicated that cathepsins might act as selectable biomarkers of hair cycle in different stages.
Introduction: Curcumin is a promising drug candidate, but its use for dermal application is limited due to its poor aqueous solubility. Thus, formulations that increase the solubility of curcumin are needed to fully exploit the therapeutic potential of curcumin. Various previous studies address this issue, but a comparison of the efficacy between these formulations remains difficult. The reason for this is a missing standard formulation as benchmark control and an easy-to-use skin penetration model that allows for a fast discrimination between different formulations.
Objective: Thus, the aims of this study were the development of a curcumin standard formulation and a screening tool that allows for a fast discrimination between the dermal penetration efficacies of curcumin from different formulations.
Methods: Ethanolic curcumin solutions were selected as simple and easy to produce standard formulations, and the ex vivo porcine ear model, coupled with epifluorescence microscopy and subsequent digital image analysis, was utilized to determine the dermal penetration efficacy of curcumin from the different formulations.
Results: Results show that the utilized skin penetration model is a suitable and versatile tool that enables not only a fast determination of the dermal penetration efficacy of curcumin from different formulations but also a detailed and mechanistic information on the fate of chemical compounds after dermal penetration. Ethanolic solutions containing 0.25% curcumin were found to be the most suitable standard formulation.
Conclusions: Results of the study provide a new, effective screening tool for the development of dermal formulations for improved dermal delivery of curcumin.
Introduction: At present, there is a lack of baseline data on the facial skin biophysical profile of women in Malaysia. The implications related to the daily habits and facial skincare product use on the skin biophysical condition are, thus, unknown. In this study, we aim to evaluate facial skin biophysical parameters of Malaysian women and examine the influence of demographic characteristics, daily habits, and facial skincare product use on these parameters.
Methods: Four skin biophysical parameters - transepidermal water loss (TEWL), melanin content, elasticity, and collagen intensity - were assessed on the cheek of the subjects (20-60 years). Demographic background, daily habits, and skincare product use were gauged through a survey. Only 197 from the 213 subjects recruited initially were used for analysis after the data were screened for normality.
Results: The biophysical parameters were similar in different races, except a higher melanin content in Indian female individuals. Elasticity and collagen intensity reduced with age, while melanin content increased in the older age-groups. But no difference was observed in TEWL at different ages. Evaluating the influence of daily habits, we observed that exercise significantly lowered TEWL and increased melanin content, which may be associated with UV radiation exposure. Facial skincare products are popular among the female subjects (>85% users). Products with moisturizing, sunscreening, and other skincare functions (astringent, antiaging, and anti-wrinkle) were preferred by subjects of all ages. These product functions significantly improve skin elasticity and reduce melanin content in the young adults. While aged women recognized the importance of having an additional skin-lightening function in their skincare routine. Although the influence of individual skincare function on skin biophysical parameters was mostly positive, the alteration of these parameters varied at different ages.
Conclusion: This is the first report of facial skin biophysical profile of Malaysian women. There is no difference among 3 major races saved for melanin content. This work demonstrated age-dependent influences on the biophysical parameters, except TEWL. The significance of skincare product use is well reflected in the improvement of these parameters at different age-groups based on individual skincare functions.
Introduction: The skin is a major physical barrier to the environment, and thus, percutaneous delivery of active ingredients to the dermal target site faces a unique set of hurdles. The efficacy of these active ingredients is governed by their release into the underlying epidermal and dermal tissue, especially when administered topically.
Objective: The aim of this study was to understand if different physicochemical properties influence the skin penetration of active ingredients and the depth to which they penetrate into the dermis.
Methods: A microdialysis (MD) setup was used to compare the percutaneous penetration in superficial and deep implanted MD membranes in porcine skin. The precise MD membrane depth was determined using histological sectioning paired with microscopy, ultrasound, and a novel computed tomographic approach.
Results: In study A, the measured depth of the superficial and deep implanted MD membranes was compared using histological sectioning, ultrasound, and computed tomography. Experimental determination of the depth up to which penetration occurs was found to be crucial to percutaneous penetration studies. In study B, the lipophilic differences of the active ingredients and its influences on the penetration was tested using hydrophilic caffeine and lipophilic LIP1 as model compounds, which have an identical molecular weight with different lipophilic characteristics. It is assumed that the lipophilic characteristics of active ingredients influence their penetration and thus governs the concentration of these molecules reaching their target site.
Conclusion: The transdermal penetration of caffeine was found to exceed that of LIP1 through the hydrophilic environment of the dermis. Thus, the findings of this study show that the precise MD dermis localization and the physicochemical properties, such as lipophilicity, influence the penetration rate of active ingredients and lay the foundation for creating optimized transdermal delivery systems.
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